| abstract |
The invention discloses the preparation method and application of a kind of amine and imines N-methyl, step is: activated carbon supported platinum catalyst A, being added in Schlenk pipe, vacuumizes after changing argon gas, solvent is added；B, phenylsilane, starting material and formic acid under protection of argon gas, are separately added into；C, entire reaction system stirs reacted at a certain temperature；D, ethyl acetate dilution after reaction, is added into system, with sodium hydrate aqueous solution quenching reaction, ethyl acetate extraction after isolating organic phase, is dried, filtered, and rotary evaporation removes solvent.Residue is chromatographed through the ethyl acetate/petroleum ether mixed solvent column of different proportion, obtains target product.Application of this method in isotope labelling pharmaceutical synthesis, catalyst amount is extremely low, and cost is very cheap, it is suitble to large-scale production, it is applicable to the amine and imines of different substituents, is suitble on the nitrogen-atoms in Structures of Natural Products easily realize methylation, prepares drug molecule. |